A xanthonoid with anticancer activity; binds covalently to SPTSSB (Ki = 1.5 µM; kinact = 0.05 min-1) and inhibits de novo sphingolipid biosynthesis; activates caspases in T47D breast cancer cells (EC50 = 0.78 µM); inhibits binding of anti-apoptotic proteins to a BH3 peptide (IC50s = 1.47

Gambogic Acid – 1 mg

Brand:
Cayman
CAS:
2752-65-0
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Gambogic acid (GA) is a xanthonoid that has been found in G. hanburyi resin and has anticancer activity.{49693,23527,23530} It binds covalently to the regulatory subunit B (SPTSSB) of the serine palmitoyltransferase complex (Ki = 1.5 µM; kinact = 0.05 min-1) and inhibits de novo sphingolipid biosynthesis.{49693} GA activates caspases in T47D breast cancer cells (EC50 = 0.78 µM) and inhibits binding of anti-apoptotic proteins to a BH3 peptide (IC50s = 1.47, 1.21, 2.02, 0.66, 1.06, and 0.79 μM for Bcl-xL, Bcl-2, Bcl-W, Bcl-B, Bfl-1, and Mcl-1, respectively), as well as decreases the expression of Bcl-2 and increases the expression of Bax in MGC-803 human gastric carcinoma cells.{23529,23528,23526} GA binds to the transferrin receptor (IC50 = 4.1 µM), reduces growth of a variety of cancer cell lines (GI50s = 0.115-1 µM), and induces apoptosis in T47D cells.{23527} It also inhibits growth of U87 glioma cells, as well as increases the levels of leucine-rich repeats and immunoglobulin-like domains protein 1 (LRIG1), decreases the levels of EGFR, and reduces Akt/mTORC1 signaling in these cells.{23530} GA inhibits the chymotrypsin activity of the 20S proteasome in a dose-dependent manner and is a slow inhibitor of inward-rectifying potassium channel 2.1 (Kir2.1; IC50 = <0.1 µM).{23531,23524}  

 

Add to quotes
SKU: - Category:

Description

A xanthonoid with anticancer activity; binds covalently to SPTSSB (Ki = 1.5 µM; kinact = 0.05 min-1) and inhibits de novo sphingolipid biosynthesis; activates caspases in T47D breast cancer cells (EC50 = 0.78 µM); inhibits binding of anti-apoptotic proteins to a BH3 peptide (IC50s = 1.47, 1.21, 2.02, 0.66, 1.06, and 0.79 μM for Bcl-xL, Bcl-2, Bcl-W, Bcl-B, Bfl-1, Mcl-1, respectively); binds to the transferrin receptor (IC50 = 4.1 µM); reduces growth of a variety of cancer cell lines (GI50s = 0.115-1 µM) and induces apoptosis in T47D cells; a slow inhibitor of inward-rectifying potassium channel 2.1 (Kir2.1; IC50 = <0.1 µM)

Formal name: 2-methyl-4-[(1R,3aS,5S,11R,14aS)-3a,4,5,7-tetrahydro-8-hydroxy-3,3,11-trimethyl-13-(3-methyl-2-buten-1-yl)-11-(4-methyl-3-penten-1-yl)-7,15-dioxo-1,5-methano-1H,3H,11H-furo[3,4-g]pyrano[3,2-b]xanthen-1-yl]-2Z-butenoic acid

Synonyms:  GA|β-Guttiferin

Molecular weight: 628.8

CAS: 2752-65-0

Purity: ≥95% (mixture of epimers)

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Natural Products||Product Type|Biochemicals|Small Molecule Activators|Caspases||Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cell Biology|Proteolysis|Cytosolic & Secreted Proteases||Research Area|Lipid Biochemistry|Sphingolipids

Related products

  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 25 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 25 mg

    Available on backorder

    Add to quotes
    View product page
  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 1 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 1 mg

    Available on backorder

    Add to quotes
    View product page
  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 500 µg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 500 µg

    Available on backorder

    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 100 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 100 mg

    Available on backorder

    Add to quotes
    View product page